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Afatinib (BIBW2992)

Alias: BIBW2992; Afatinib free base; BIBW 2992; BIBW 2992; Afatinib; trade name: Gilotrif, Tomtovok and Tovok
Cat No.:V0536 Purity: ≥98%
Afatinib (formerly BIBW 2992; BIBW-2992; brand name: Gilotrif), is a potent, covalent/irreversible, and orally bioavailable dual (EGFR/ErbB) receptor tyrosine kinase (RTK) inhibitor with anticancer activity.
Afatinib (BIBW2992)
Afatinib (BIBW2992) Chemical Structure CAS No.: 850140-72-6
Product category: EGFR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Afatinib (BIBW2992):

  • Afatinib (BIBW2992) Dimaleate
  • Afatinib-d6 dimaleate (BIBW 2992MA2-d6)
  • Afatinib D6
  • Afatinib oxalate
  • (R)-Afatinib ((R)-BIBW 2992)
  • Afatinib-d4 (BIBW 2992-d4)
Official Supplier of:
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Top Publications Citing lnvivochem Products
InvivoChem's Afatinib (BIBW2992) has been cited by 1 publication
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Afatinib (formerly BIBW 2992; BIBW-2992; brand name: Gilotrif), is a potent, covalent/irreversible, and orally bioavailable dual (EGFR/ErbB) receptor tyrosine kinase (RTK) inhibitor with anticancer activity. Afatinib is an FDA-approved anticancer medication used to treat lung cancer that is not small cell (NSCLC). In the USA, Gilotrif is the brand name under which it is sold. It is 100 times more active against the Gefitinib-resistant L858R-T790M EGFR mutant. It irreversibly binds to and inhibits EGFR/HER2, including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M), and HER2. In cell-free assays, its IC50 values are 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively.

Biological Activity I Assay Protocols (From Reference)
Targets
EGFRL858R (IC50 = 0.4 nM); EGFR (wt) (IC50 = 0.5 nM); ErbB4 (IC50 = 1 nM); EGFRL858R/T790M (IC50 = 10 nM); HER2 (IC50 = 14 nM)
ln Vitro
BIBW2992 exhibits potent inhibition of EGFR and HER2 in both wild-type and mutant forms. It has comparable potency to gefitinib against L858R EGFR, but it is approximately 100 times more active against the L858R-T790M EGFR double mutant that is resistant to gefitinib. In vivo, BIBW2992 demonstrates strong effects on the phosphorylation of both EGFR and HER2. When compared to reference compounds (like Lapatinib et al.), it performs well in all tested cell types, including human epidermoid carcinoma cell line A431 that expresses EGFR, murine NIH-3T3 cells transfected with HER2, breast cancer cell line BT-474, and gastric cancer cell line NCI-N87 that express endogenous HER2.[1]
ln Vivo
Afatinib (0-20 mg/kg, Orally, daily for 25 days) exhibits a significant decrease in tumor growth and phosphorylation of AKT, HER2, EGFR, and HER3.
Afatinib (15 mg/kg, Orally, in a schedule of 5 days on plus 2 days off, for two weeks) strongly inhibits the growth of HKESC-2 tumor.
Enzyme Assay
The human EGFR wild type and EGFR L858R/T790M double mutant tyrosine kinase domains are fused to GST and extracted. Next, enzyme activity is measured with and without the inhibitor BIBW2992, which is serially diluted in 50% DMSO. Biotinylated pEY (bio-pEY) is added as a tracer substrate and a random polymer, pEY (4:1), is used as the substrate. Utilizing the baculovirus system, the HER2 kinase domain is cloned and extracted in a manner akin to that of EGFR kinase. Supplementary information contains specifics about the assays conducted for EGFR, HER2, SRC, BIRK, and VEGFR2 kinase activity.
Cell Assay
For the EGFR phosphorylation test, 1 × 104 NSCLC cells are plated into each well of a 96-well plate and grown for an entire night in serum-free medium. The following day, the plates are incubated at 37 °C for one hour following the addition of BIBW2992. EGF stimulation is carried out at room temperature for 10 minutes using 100 ng/mL. Following an hour of shaking at room temperature and an extraction using 120 μL of HEPEX buffer per well, the cells are cleaned with ice-cold PBS. HER2 phosphorylation assay uses 2 × 104 cells per well in total. The c-erb2/HER2 oncoprotein Ab-5(Clone N24)-Biotin and anti-EGFR-Biotin are coated on streptavidin precoated plates at a 1:100 dilution in blocking buffer. Once in the antibody-coated wells, cell extracts are allowed to sit at room temperature for one hour. Measurement of extinction occurs at 450 nm.
Animal Protocol
Athymic NMRI-nu/nu female mice[1]
20 mg/kg
Oral administration
Four bitransgenic mice on continuous doxycycline diets for more than 6 weeks were subjected to MRI (Figure 4) to document the lung tumor burden. Afatinib (BIBW2992) formulated in 0.5% methocellulose-0.4% polysorbate-80 (Tween 80) was administered orally by gavage at 20 mg/kg once daily dosing schedule. Rapamycin was dissolved in 100% ethanol, freshly diluted in 5% PEG400 and 5% Tween 80 before treatment and administered by intraperitoneal injection at 2 mg/kg daily dosage. Mice were monitored by MRI every 1 or 2 weeks to determine reduction in tumor volume and killed for further histological and biochemical studies after drug treatment. For immunohistochemistry staining, three tumor-bearing mice in each group were treated three times with either Afatinib (BIBW2992) (20 mg/kg) alone or Afatinib (BIBW2992) (20 mg/kg) and rapamycin 2 mg/kg at 24 h intervals and killed 1 h after the last drug delivery. All the mice were kept on the doxycycline diet throughout the experiments. Littermates were used as controls.[1]
ADME/Pharmacokinetics
Absorption, Distribution and Excretion
Following oral administration, time to peak plasma concentration (Tmax) is 2 to 5 hours. Maximum concentration (Cmax) and area under the concentration-time curve from time zero to infinity (AUC0-∞) values increased slightly more than dose proportional in the range of 20 to 50 mg. The geometric mean relative bioavailability of 20 mg tablets was 92% as compared to an oral solution. Additionally, systemic exposure to afatinib is decreased by 50% (Cmax) and 39% (AUC0-∞), when administered with a high-fat meal compared to administration in the fasted state. Based on population pharmacokinetic data derived from clinical trials in various tumor types, an average decrease of 26% in AUCss was observed when food was consumed within 3 hours before or 1 hour after taking afatinib.
In humans, excretion of afatinib is primarily via the feces. Following administration of an oral solution of 15 mg afatinib, 85.4% of the dose was recovered in the feces and 4.3% in urine. The parent compound afatinib accounted for 88% of the recovered dose.
The volume of distribution of afatinib recorded in healthy male volunteers is documented as 4500 L. Such a high volume of distribution in plasma suggests a potentially high tissue distribution.
The apparent total body clearance of afatinib as recorded in healthy male volunteers is documented as being a high geometric mean of 1530 mL/min.
Metabolism / Metabolites
Enzyme-catalyzed metabolic reactions play a negligible role for afatinib in vivo. Covalent adducts to proteins were the major circulating metabolites of afatinib.
Biological Half-Life
Afatinib is eliminated with an effective half-life of approximately 37 hours. Thus, steady-state plasma concentrations of afatinib were achieved within 8 days of multiple dosing of afatinib resulting in an accumulation of 2.77-fold (AUC0-∞) and 2.11-fold (Cmax). In patients treated with afatinib for more than 6 months, a terminal half-life of 344 h was estimated.
Toxicity/Toxicokinetics
Hepatotoxicity
Elevations in serum aminotransferase levels are common during afatinib therapy occurring in 20% to 50% of patients, but rising above 5 times the upper limit of the normal range in only 1% to 2%. Hepatic failure is said to have occurred in 0.2% of patients and to have resulted in several fatalities. Hepatotoxicity appears to be a class effect among protein kinase inhibitors of EGFR2, although liver injury appears to be more frequent and more severe with gefitinib than with afatinib and erlotinib. Specific details of the liver injury associated with afatinib such as latency, serum enzyme pattern, clinical features and course, have not been published. Other EGFR inhibitors, such as erlotinib and gefitinib typically cause liver injury arising within days or weeks of starting therapy and presenting abruptly with hepatocellular enzyme elevations and a moderate-to-severe course. Immunoallergic and autoimmune features are not common. The rate of clinically significant liver injury and hepatic failure is increased in patients with preexisting cirrhosis or hepatic impairment due to liver tumor burden.
Likelihood score: D (possible cause of clinically apparent liver injury).
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the clinical use of afatinib during breastfeeding. Because afatinib is about 95% bound to plasma proteins, the amount in milk is likely to be low. However, its half-life is about 37 hours and it might accumulate in the infant. the manufacturer recommends that breastfeeding be discontinued during afatinib therapy and for 2 weeks after the last dose.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.
Protein Binding
In vitro binding of afatinib to human plasma proteins is approximately 95%. Afatinib binds to proteins both non-covalently (traditional protein binding) and covalently.
References

[1]. Oncogene . 2008 Aug 7;27(34):4702-11.

[2]. Expert Opin Investig Drugs . 2014 Jan;23(1):135-43.

Additional Infomation
Pharmacodynamics
Aberrant ErbB signaling triggered by receptor mutations, and/or amplification, and/or receptor ligand overexpression contributes to the malignant phenotype. Mutation in EGFR defines a distinct molecular subtype of lung cancer. In non-clinical disease models with ErbB pathway deregulation, afatinib as a single agent effectively blocks ErbB receptor signaling resulting in tumor growth inhibition or tumor regression. NSCLC tumors with common activating EGFR mutations (Del 19, L858R) and several less common EGFR mutations in exon 18 (G719X) and exon 21 (L861Q) are particularly sensitive to afatinib treatment in non-clinical and clinical settings. Limited non-clinical and/or clinical activity was observed in NSCLC tumors with insertion mutations in exon 20. The acquisition of a secondary T790M mutation is a major mechanism of acquired resistance to afatinib and gene dosage of the T790M-containing allele correlates with the degree of resistance in vitro. The T790M mutation is found in approximately 50% of patients' tumors upon disease progression on afatinib, for which T790M targeted EGFR TKIs may be considered as a next line treatment option. Other potential mechanisms of resistance to afatinib have been suggested preclinically and MET gene amplification has been observed clinically. At the same time, the effect of multiple doses of afatinib (50 mg once daily) on cardiac electrophysiology and the QTc interval was evaluated in an open-label, single-arm study in patients with relapsed or refractory solid tumors. Ultimately, no large changes in the mean QTc interval (i.e., >20 ms) were detected in the study.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H25CLFN5O3
Molecular Weight
485.94
Exact Mass
485.162
Elemental Analysis
C, 59.32; H, 5.19; Cl, 7.30; F, 3.91; N, 14.41; O, 9.88
CAS #
850140-72-6
Related CAS #
Afatinib dimaleate;850140-73-7;Afatinib-d6;1313874-96-2;Afatinib oxalate;1398312-64-5;(R)-Afatinib;439081-17-1;Afatinib-d4
PubChem CID
10184653
Appearance
White to light yellow solid powder
Density
1.4±0.1 g/cm3
Boiling Point
676.9±55.0 °C at 760 mmHg
Melting Point
100 - 102 °C
Flash Point
363.2±31.5 °C
Vapour Pressure
0.0±2.1 mmHg at 25°C
Index of Refraction
1.668
LogP
3.59
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
8
Heavy Atom Count
34
Complexity
702
Defined Atom Stereocenter Count
1
SMILES
N(C1C=CC(F)=C(Cl)C=1)C1=NC=NC2=CC(=C(C=C12)NC(=O)/C=C/CN(C)C)O[C@@H]1COCC1
InChi Key
ULXXDDBFHOBEHA-CWDCEQMOSA-N
InChi Code
InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
Chemical Name
(E)-N-[4-(3-chloro-4-fluoroanilino)-7-[(3S)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide
Synonyms
BIBW2992; Afatinib free base; BIBW 2992; BIBW 2992; Afatinib; trade name: Gilotrif, Tomtovok and Tovok
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~97 mg/mL (~199.6 mM)
Water: <1 mg/mL
Ethanol: ~15 mg/mL (~30.9 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.14 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.


Solubility in Formulation 4: 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 10 mg/mL

Solubility in Formulation 5: 5 mg/mL (10.29 mM) in 0.5% Methylcellulose/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0579 mL 10.2893 mL 20.5787 mL
5 mM 0.4116 mL 2.0579 mL 4.1157 mL
10 mM 0.2058 mL 1.0289 mL 2.0579 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
Sotorasib Activity in Subjects With Advanced Solid Tumors With KRAS p.G12C Mutation (CodeBreak 101)
CTID: NCT04185883
Phase: Phase 1    Status: Recruiting
Date: 2024-11-29
Dual Inhibition of EGFR With Afatinib and Cetuximab in the Treatment of Advanced Squamous Cell Cancers of the Head and Neck
CTID: NCT02979977
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-26
Afatinib in Patients with Fanconi Anemia (FA) and Advanced Head and Neck Squamous Cell Carcinoma (HNSCC)
CTID: NCT06648096
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-20
Afatinib With CT and RT for EGFR-Mutant NSCLC
CTID: NCT01553942
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-20
Pemigatinib + Afatinib in Advanced Refractory Solid Tumors
CTID: NCT06302621
Phase: Phase 1    Status: Recruiting
Date: 2024-11-18
View More

Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
CTID: NCT02465060
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-18


Trastuzumab Deruxtecan(T-DXd) and Afatinib Combination in HER2-low Advanced Gastric Cancer
CTID: NCT06085755
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-06
The Study Observes Afatinib as First-line Treatment in Patients With Epidermal Growth Factor Receptor (EGFR) Mutation-positive Advanced Non-small Cell Lung Cancer
CTID: NCT04206787
Phase:    Status: Completed
Date: 2024-11-05
LUX-Head&Neck 3: Afatinib (BIBW2992) Versus Methotrexate for the Treatment of Recurrent and/or Metastatic Head and Neck Squamous Cell Cancer After Platinum Based Chemotherapy
CTID: NCT01856478
Phase: Phase 3    Status: Active, not recruiting
Date: 2024-10-31
Target Therapy With GEMOX in Recectable Gallbladder Carcinoma Patients Monitored by ctDNA
CTID: NCT04183712
Phase: Phase 2    Status: Recruiting
Date: 2024-10-16
Study Evaluating Zenocutuzumab in Patients with or Without Molecularly Defined Cancers
CTID: NCT05588609
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-10-03
Phase 1/2 Study of MRTX849 in Patients With Cancer Having a KRAS G12C Mutation KRYSTAL-1
CTID: NCT03785249
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-09-20
Real-World Effectiveness of Afatinib (Gilotrif) Following Immunotherapy in the Treatment of Metastatic, Squamous Cell Carcinoma of the Lung: A Multi-Site Retrospective Chart Review Study in the U.S.
CTID: NCT04750824
Phase:    Status: Completed
Date: 2024-09-19
A Study to Learn About the Effectiveness of Cancer Medicines in Patients With Metastatic Non-small Cell Lung Cancer in Norway.
CTID: NCT05834348
Phase:    Status: Completed
Date: 2024-09-04
A Phase II Evaluation of Afatinib in Patients With Persistent or Recurrent HER2-positive Uterine Serous Carcinoma
CTID: NCT02491099
Phase: Phase 2    Status: Recruiting
Date: 2024-08-20
Study of Afatinib in Advanced Cutaneous Squamous Cell Carcinoma
CTID: NCT05070403
Phase: Phase 2    Status: Recruiting
Date: 2024-08-02
Low-dose Radiotherapy Plus Tislelizumab in Combination With Afatinib for Neoadjuvant Treatment of Surgically Resectable Head and Neck Squamous Carcinoma
CTID: NCT06494189
Phase: Phase 1    Status: Recruiting
Date: 2024-07-10
Phase 2 Trial of Afatinib Plus Prednisone for Advanced Squamous NSCLC
CTID: NCT04497584
Phase: Phase 2    Status: Recruiting
Date: 2024-07-09
Pilot Trial for Treatment of Recurrent Glioblastoma
CTID: NCT05432518
PhaseEarly Phase 1    Status: Recruiting
Date: 2024-06-03
Observational Study of Afatinib 30 mg Daily
CTID: NCT04909073
Phase:    Status: Recruiting
Date: 2024-05-17
Study of EGFR TKI in Patients With Advanced NSCLC Harbouring EGFR Mutations
CTID: NCT06062823
Phase: Phase 2    Status: Recruiting
Date: 2024-05-17
Testing Afatinib as Potentially Targeted Treatment in Cancers With EGFR Genetic Changes (MATCH - Subprotocol A)
CTID: NCT06385483
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-05-06
Afatinib in Advanced NRG1-Rearranged Malignancies
CTID: NCT04410653
Phase: Phase 2    Status: Completed
Date: 2024-04-05
An Open Label Trial of Afatinib (Giotrif) in Treatment-naive (1st Line) or Chemotherapy Pre-treated Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC) Harboring EGFR Mutation(s)
CTID: NCT01853826
Phase: Phase 3    Status: Completed
Date: 2024-03-26
Safety Study of Afatinib and Postoperative Radiation Therapy to Treat Head and Neck Cancer
CTID: NCT01783587
Phase: Phase 1    Status: Completed
Date: 2024-03-06
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial
CTID: NCT03878524
Phase: Phase 1    Status: Terminated
Date: 2024-03-04
Treatment With BIBW 2992, Irreversible Inhibitor of EGFR and HER-2 in Non-small Cell Lung Cancer
CTID: NCT01542437
Phase: Phase 2    Status: Completed
Date: 2024-02-06
Cambridge Brain Mets Trial 1
CTID: NCT02768337
Phase: Phase 1/Phase 2    Status: Terminated
Date: 2024-01-31
The Drug Rediscovery Protocol (DRUP Trial)
CTID: NCT02925234
Phase: Phase 2    Status: Recruiting
Date: 2024-01-24
Neoadjuvant Chemotherapy, Tislelizumab With Afatinib for HNSCC
CTID: NCT05516589
Phase: Phase 2    Status: Recruiting
Date: 2023-12-29
Neoadjuvant Tislelizumab With Afatinib for Resectable Head and Neck Squamous Cell Carcinoma
CTID: NCT05517330
Phase: Phase 2    Status: Recruiting
Date: 2023-12-29
Study Assessing Activity of Molecularly Matched Targeted Therapies in Select Tumor Types Based on Genomic Alterations
CTID: NCT02795156
Phase: Phase 2    Status: Completed
Date: 2023-12-05
Deciphering Afatinib Response and Resistance With INtratumour Heterogeneity
CTID: NCT02183883
Phase: Phase 2    Status: Completed
Date: 2023-11-29
Biomarker-based Study in R/M SCCHN
CTID: NCT03088059
Phase: Phase 2    Status: Active, not recruiting
Date: 2023-11-03
Non-interventional Study for Real-world Data of Afatinib Treatment in First-line Setting and of Subsequent Therapies for Patients With Advanced Epidermal Growth Factor Receptor (EGFR) Mutation-positive Lung Adenocarcinoma
CTID: NCT04795245
Phase:    Status: Completed
Date: 2023-10-31
Afatinib and Cetuximab in Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Positive Non-small-cell Lung Cancer
CTID: NCT03727724
Phase: Phase 2    Status: Completed
Date: 2023-10-18
A Study of Afatinib in Patients With Advanced Cancer With Changes in the HER Gene
CTID: NCT02506517
Phase: Phase 2    Status: Completed
Date: 2023-08-01
Afatinib After Chemoradiation and Surgery in Treating Patients With Stage III-IV Squamous Cell Carcinoma of the Head and Neck at High-Risk of Recurrence
CTID: NCT01824823
Phase: Phase 2    Status: Terminated
Date: 2023-06-28
AFAMOSI: Efficacy and Safety of Afatinib Followed by Osimertinib Compared to Osimertinib in Patients With EGFRmutated/T790M Mutation Negative Nonsquamous NSCLC
CTID: NCT04413201
Phase: Phase 4    Status: Active, not recruiting
Date: 2023-06-02
Palbociclib Combined With Afatinib for Advanced Squamous Carcinoma of Esophagus or Gastroesophageal Junction
CTID: NCT05865132
Phase: Phase 2    Status: Recruiting
Date: 2023-05-18
Dry Pleurodesis With Talcum and Afatinib is Used to Treat Patients With Non-Small Cell Lung Carcinoma
CTID: NCT03827070
Phase: Phase 1    Status: Active, not recruiting
Date: 2023-04-25
To Evaluate the Efficacy and Safety of Afatinib for Advanced ALTRK-negative ESCC
CTID: NCT05818982
Phase: Phase 2    Status: Recruiting
Date: 2023-04-19
Primary Tumor Resection With EGFR TKI for Stage IV NSCLC
CTID: NCT05215548
Phase: Phase 2    Status: Recruiting
Date: 2023-04-04
Phase II Study of Afatinib Plus Bevacizumab in the Treatment Epidermal Growth Factor Receptor (EGFR) Exon G719X, S768I, and L861Q Mutation Metastatic Non-Small Cell Lung Cancer
CTID: NCT05267288
Phase: Phase 2    Status: Recruiting
Date: 2023-03-29
Afatinib, Paclitaxel, 2nd Line, Advanced Gastric Cancer
CTID: NCT02501603
Phase: Phase 2    Status: Completed
Date: 2023-01-27
Neoadjuvant Afatinib Therapy for Potentially Resectable Stage III EGFR Mutation-Positive Lung Adenocarcinoma
CTID: NCT04201756
Phase: Phase 2    Status: Completed
Date: 2022-12-23
Phase II Umbrella Study Directed by Next Generation Sequencing
CTID: NCT03574402
Phase: Phase 2    Status: Recruiting
Date: 2022-12-06
Afatinib (GILOTRIF®) in Patients Suffering From Tumors Harboring Neuregulin 1 (NRG1) Gene Alterations (Specifically NRG1 Gene Fusion-positive Advanced Solid Tumors)
CTID: NCT05107193
Phase:    Status: No longer available
Date: 2022-11-08
Study to Evaluate the Efficacy of Afatinib in Skull Base Chordoma
CTID: NCT05519917
Phase: Phase 2    Status: Not yet recruiting
Date: 2022-09-30
Afatinib in NSCLC With HER2 Mutation
CTID: NCT02369484
Phase: Phase 2    Status: Completed
Date: 2022-08-24
Combination of Cetuximab With Afatinib for Patient With EGFR Mutated Lung Cancer
CTID: NCT02716311
Phase: Phase 2    Status: Completed
Date: 2022-08-11
BIBW 2992 (Afatinib) for the Treatment of Patients With HER2-positive, Hormone-refractory Prostate Cancer
CTID: NCT01320280
Phase: Phase 2    Status: Terminated
Date: 2022-07-01
Afatinib on CNS Metastases and LMD in EGFR Mutation Positive NSCLC
CTID: NCT03711422
Phase: Phase 1    Status: Terminated
Date: 2022-06-14
Evaluate the Impact of Afatinib on Quality of Life and Symptom Burden of Greek Subjects With Advanced NSCLC in Routine Patient Care Settings
CTID: NCT02440854
Phase:    Status: Completed
Date: 2022-04-27
Afatinib and Pembrolizumab for Head and Neck Squamous Cell Carcinoma (ALPHA Study)
CTID: NCT03695510
Phase: Phase 2    Status: Completed
Date: 2022-04-21
Afatinib in Locally Advanced and Metastatic Chordoma
CTID: NCT03083678
Phase: Phase 2    Status: Unknown status
Date: 2022-04-20
Afatinib and Necitumumab in Patients With EGFR Mutation Positive Advanced or Metastatic Non-small Cell Lung Cancer
CTID: NCT03054038
Phase: Phase 1    Status: Terminated
Date: 2022-04-14
BIBW 2992 Plus Simvastatin vs. BIBW 2992 in Previously Treated Patients With Advanced Non-adenocarcinomatous NSCLC
CTID: NCT01156545
Phase: Phase 2    Status: Completed
Date: 2022-04-06
Safety Study of Afatinib for Brain Cancer
CTID: NCT02423525
Phase: Phase 1    Status: Completed
Date: 2022-03-10
Efficacy and Safety of Precision Therapy in Refractory Tumor
CTID: NCT03239015
Phase: Phase 2    Status: Unknown status
Date: 2022-03-04
Research of Biomarkers of Activity and Efficacy of BIBW2992 in Untreated Non-metastatic HNSCC Patients
CTID: NCT01415674
Phase: Phase 2    Status: Completed
Date: 2022-02-02
JMT101 Combined With Afatinib in Patients With Advanced Esophageal Squamous Cell Carcinoma After Standard Therapy
CTID: NCT05164848
Phase: Phase 1    Status: Unknown status
Date: 2021-12-21
Safety, Tolerability and Efficacy of Vaginal Suppositories for Treatment of the Endometriosis
CTID: NCT03481842
Phase: Phase 1/Phase 2    Status: Withdrawn
Date: 2021-10-29
Afatinib in Lung Cancer With EGFR Mutation From Circulating Tumor DNA
CTID: NCT02629523
Phase: Phase 2    Status: Completed
Date: 2021-08-03
Afatinib Plus Toripalimab in Previously Treated ESCC With EGFR Overexpression or EGFR Amplification
CTID: NCT04880811
Phase: Phase 2    Status: Unknown status
Date: 2021-07-13
Evaluation of Afatinib in Maintenance Therapy in Squamous Cell Carcinoma of the Head and Neck
CTID: NCT01427478
Phase: Phase 3    Status: Completed
Date: 2021-06-01
Trial of Afatinib in Pediatric Tumours
CTID: NCT02372006
Phase: Phase 1/Phase 2    Status: Completed
Date: 2021-03-04
Testing Afatinib in Combination With Pembrolizumab in Patients With Squamous Cell Carcinoma of the Lung
CTID: NCT03157089
Phase: Phase 2    Status: Completed
Date: 2021-02-23
Afatinib Osimertinib Sequencing NIS
CTID: NCT03370770
Phase:    Status: Completed
Date: 2020-12-24
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The effects of the proton pump inhibitor esomeprazole on the bioavailability of afatinib (Giotrif®) in patients with non-small cell lung cancer (NSCLC) 'the BIO-GIO study'
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2017-07-05
Precision 2: an open explorative phase II, open label study of afatinib in the treatment of advanced cancer carrying an EGFR, a HER2 or a HER3 mutation.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2017-06-21
Phase II open label single arm exploratory trial of oral afatinib monotherapy following platinum failure for patients with advanced/metastatic urothelial tract carcinoma with ERBB receptor deregulation.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2016-04-29
Phase II trial of Afatinib as induction treatment in patients with stage IIIA or stage IIIB N2 requiring neoadjuvant treatment for pN2 non squamous non small cell lung cancer (NSCLC) with EGFR-activating mutations.
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2016-04-26
Phase II study evaluating the combination of cetuximab with afatinib as first-line treatment for patients with EGFR mutated Non Small Cell Lung Cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2015-11-20
A randomised, double blind phase I/II trial to investigate efficacy, immunogenicity and safety of intradermally administered BI 1361849 (CV9202) plus afatinib versus placebo plus afatinib as first-line treatment for patients with stage IV adenocarcinoma of the lung harbouring common EGFR mutations.
CTID: null
Phase: Phase 1, Phase 2    Status: Prematurely Ended, Completed
Date: 2015-11-19
Maintaining ERBB blockade in EGFR-mutated lung cancer (MARBLE) - A randomized, open-label, phase II study of maintaining pan-ERBB blockade following platinum-based induction chemotherapy in patients with EGFR mutated, metastatic non-small-cell lung cancer progressing after treatment with afatinib as first EGFR-targeting agent.
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2015-06-29
Afatinib in pretreated patients with advanced NSCLC harbouring HER2 exon 20 mutations
CTID: null
Phase: Phase 2    Status: Completed
Date: 2015-05-18
Phase I/II open label, dose escalation trial to determine the MTD, safety, PK and efficacy of afatinib monotherapy in children aged ≥ 1 year to <18 years with recurrent/refractory neuroectodermal tumours, rhabdomyosarcoma and/or other solid tumours with known ErbB pathway deregulation regardless of tumour histology
CTID: null
Phase: Phase 1, Phase 2    Status: GB - no longer in EU/EEA, Temporarily Halted, Completed
Date: 2015-04-18
Phase I/II study with the combination of afatinib and selumetinib in advanced KRAS mutant positive and PIK3CA wildtype non-small cell lung cancer and colorectal cancer
CTID: null
Phase: Phase 1, Phase 2    Status: Ongoing
Date: 2015-01-14
An open label, single-arm phase IV study to assess the efficacy and safety of afatinib as second-line therapy for patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harbouring an EGFR mutation (Del19 or L858R) who have failed first-line treatment with platinum-based chemotherapy
CTID: null
Phase: Phase 4    Status: Completed
Date: 2014-12-17
A randomized open-label Phase II study of letrozole plus afatinib (BIBW2992) versus letrozole alone in first-line treatment of advanced ER+, HER2- postmenopausal breast cancer with low ER expression
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-10-17
An open label trial of afatinib (Giotrif) in treatment-naive (1st line) or chemotherapy pre-treated patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring EGFR mutation(s)
CTID: null
Phase: Phase 3    Status: Ongoing, Completed
Date: 2013-06-25
Etude de phase II, randomisée, multicentrique, de l’Afatinib (BIBW2992) administré en pré-opératoire, chez des patients ayant un carcinome épidermoïde des voies aérodigestives supérieures non métastatique, en vue d'identifier des biomarqueurs prédictifs et/ou pharmacodynamiques de l'activité biologique et de l'efficacité
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-05-28
An Open Label Multi-Centre Preoperative Window of Opportunity Study of Afatinib in Stage Ia to IIb Non-Small Cell Lung Cancer
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2013-01-25
Gemcitabine in Combination with the Oral Irreversible ErbB Inhibitor Afatinib versus Gemcitabine Alone in Patients with Metastatic Pancreatic Cancer: an Explorative Randomized Phase II Trial
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-01-17
A Phase II, single-arm clinical trial of administration of cisplatin and 5-fluorouracil with afatinib as first-line therapy in patients with inoperable gastric or gastroesophageal junction cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2012-10-24
Neoadjuvant BIBW 2992 followed by surgery in squamous cell carcinoma of the head and neck: an EORTC NOCI-HNCG window study.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2012-06-07
A multicentric randomized phase II study evaluating dual targeting of the EGFR using the combination of cetuximab and afatinib versus cetuximab alone in patients with chemotherapy refractory wtKRAS metastatic colorectal cancer.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2012-05-29
LUX-Lung 8: A randomized, open-label Phase III trial of afatinib versus erlotinib in patients with advanced squamous cell carcinoma of the lung as second-line therapy following first-line platinum-based chemotherapy
CTID: null
Phase: Phase 3    Status: Completed
Date: 2012-02-22
Single-arm, open-label, multicentre phase II study evaluating the efficacy and safety of BIBW 2992 (Afatinib) in combination with vinorelbine for the treatment of patients with metastatic breast cancer with intermediate HER2 expression (HER2 2+ by immunohistochemistry, fluorescence in-situ hybridisation (FISH) negative) after failure of first-line therapy in the metastatic setting and having been pre-treated with anthracyclines
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2012-02-13
LUX-Lung 7: A randomised, open-label Phase IIb Trial of afatinib versus gefitinib as first-line treatment of patients with EGFR mutation positive advanced adenocarcinoma of the lung
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-12-29
Trial of afatinib (BIBW 2992) in suspected or confirmed mutant EGFR lung cancer patients unfit for chemotherapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-12-19
LUX-Head & Neck 1
CTID: null
Phase: Phase 3    Status: Completed
Date: 2011-10-25
Randomised phase II study of afatinib alone or in combination with vinorelbine versus investigator’s choice of treatment in patients with HER2-positive breast cancer with progressive brain metastases after trastuzumab or lapatinib based therapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-09-14
A randomized, double-blind, placebo-controlled, phase III study to evaluate the efficacy of afatinib (BIBW 2992) in maintenance therapy after postoperative concurrent radiotherapy and chemotherapy for squamous-cell carcinoma of the head and neck : a GORTEC collaborative group study 2010-02
CTID: null
Phase: Phase 3    Status: Completed
Date: 2011-08-11
LUX-Head & Neck 2
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2011-07-27
An open label, phase II trial of afatinib with or without vinorelbine for
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-07-21
Single-arm, open-label, monocentric Phase II study evaluating the efficacy and safety of BIBW 2992 (Afatinib) for the treatment of patients with HER2-positive, hormone-refractory prostate cancer after failure of treatment with docetaxel or ineligible for treatment with docetaxel
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2011-06-20
LUX-Breast 2;An open label, phase II trial of BIBW 2992 (afatinib) in patients with metastatic HER2-overexpressing breast cancer failing HER2-targeted treatment in the neoadjuvant and/or adjuvant treatment setting
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-02-18
LUX-Breast 1; An open label, randomised phase III trial of BIBW 2992 and vinorelbine versus trastuzumab and vinorelbine in patients with metastatic HER2-overexpressing breast cancer failing one prior trastuzumab treatment
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2010-05-17
An open label, partially randomised Phase II trial to investigate the efficacy and safety of BIBW 2992 in patients with metastatic colorectal cancer who never received prior anti-EGFR treatment
CTID: null
Phase: Phase 2    Status: Completed
Date: 2010-05-13
Phase III randomized trial of BIBW 2992 plus weekly paclitaxel versus
CTID: null
Phase: Phase 3    Status: Completed
Date: 2010-03-02
A phase Ib open label clinical trial of continuous once daily oral treatment using BIBW 2992 plus cetuximab (Erbitux®) in patients with non-small cell lung cancer with progression following prior erlotinib (Tarceva®) or gefitinib (Iressa®)
CTID: null
Phase: Phase 1, Phase 2    Status: Completed
Date: 2010-02-09
LUX-Lung 3; A randomised, open-label, phase III study of BIBW 2992 versus chemotherapy as first-line treatment for patients with stage IIIB or IV adenocarcinoma of the lung harbouring an EGFR activating mutation
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2009-09-28
A randomized, open-label Phase II study of BIBW 2992 versus cetuximab (Erbitux®) in patients with metastatic or recurrent Head and Neck Squamous Cell Carcinoma (HNSCC) after failure of platinum-containing therapy with a cross-over period for progressing patients.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2009-05-07
Phase II open label trial to assess the efficacy and the impact on QTcF of continuous oral BIBW 2992 at a daily dose of 50 mg in patients with relapsed or refractory solid tumours including patients with brain metastases and those with glioblastoma not amenable to other therapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2009-03-16
A Phase II single-arm trial of BIBW 2992(Tovok) in EGFR FISH positive non-small cell lung cancer patients
CTID: null
Phase: Phase 2    Status: Completed
Date: 2008-11-20
A Phase II single-arm trial of BIBW 2992 in demographically and genotypically selected non-small cell lung cancer patients
CTID: null
Phase: Phase 2    Status: Completed
Date: 2008-06-13
Phase IIb/III randomized, double-blind trial of BIBW 2992 plus best
CTID: null
Phase: Phase 2, Phase 3    Status: Completed
Date: 2008-05-13
Phase II trial of BIBW 2992 in patients with HER2-positive metastatic breast cancer after failure of trastuzumab therapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2007-10-31
A multicenter, randomized, open label phase II trial evaluating the efficacy and safety of mFOLFOX7 plus weekly alternating sequential oral administration of BIBF 1120 250 mg twice daily and BIBW 2992 50 mg once daily (BB) versus mFOLFOX7 alone as first-line therapy in patients with metastatic colorectal cancer.
CTID: null
Phase: Phase 2    Status: Completed, Prematurely Ended
Date: 2007-01-22
A phase II study of BIBW 2992 added to letrozole in patients with estrogen receptor positive hormone refractory metastatic breast cancer progressing on letrozole
CTID: null
Phase: Phase 2    Status: Completed
Date: 2006-12-07
An open label phase II trial to assess the efficacy and safety of a once daily oral dose of 50 mg BIBW 2992 in two cohorts of patients with HER2-negative metastatic breast cancer after failure of no more than two chemotherapy regimen
CTID: null
Phase: Phase 2    Status: Completed, Prematurely Ended
Date: 2006-10-31
A multi-centre 3-arm randomized phase II trial of BIBF 1120 versus BIBW 2992 versus sequential administration of BIBF 1120 and BIBW 2992 in patients with hormone-resistant prostate cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2006-02-16
Dual blockage with Afatinib and Trastuzumab as neooadjuvant treatment for patients with lo-cally advanced or operable breast cancer receiving taxane-anthracycline containing chemo-therapy (DAFNE study).
CTID: null
Phase: Phase 2    Status: Completed
Date:
First-line afatinib for elderly patients
CTID: jRCTs031180136
Phase:    Status: Complete
Date: 2019-02-19
Afatinib translational study in patients with EGFR mutation-positive non-squamous non-small cell lung cancer acquired resistance to osimertinib
CTID: jRCTs071180013
Phase:    Status: Not Recruiting
Date: 2019-01-24
Trial of the alternative therapy with osimeritinib and afatinib for NSCLC with EGFR mutation (Alt trial) (WJOG10818L)
CTID: jRCTs051180009
Phase:    Status: Complete
Date: 2018-11-26
Afa+Bev for EGFR mutant NSCLC
CTID: jRCTs061180006
Phase:    Status: Complete
Date: 2018-11-19
A phase I study; Afatinib in Combination of Osimertinib in patients with Relapsed Non-Small Cell Lung Cancer after failure of prior Osimertinib
CTID: jRCTs051180008
Phase:    Status: Complete
Date: 2018-11-08
Prospective study to investigate the resistant mechanism to afatinib treatment in EGFR mutation-positive non-small cell lung cancer
CTID: UMIN000031845
Phase:    Status: Complete: follow-up complete
Date: 2018-03-22
A phase I study Afatinib in Combination of Osimertinib in patients with Relapsed Non-Small Cell Lung Cancer after failure of prior Osimertinib
CTID: UMIN000031501
Phase:    Status: Complete: follow-up complete
Date: 2018-03-09
Multicenter, prospective interventional study to evaluate therapeutic effect of Afatinib in patients with advanced non-small cell lung cancer, EGFR mutation positive and brain metastasis
CTID: UMIN000031117
Phase:    Status: Complete: follow-up complete
Date: 2018-02-03
Afatinib plus Bevacizumab Combination after osimertinib failure for aDvanced EGFR-mutant non-small cell lung cancer: a multicenter prospective single arm phase II study (ABCD-study)
CTID: UMIN000030545
Phase: Phase II    Status: Recruiting
Date: 2018-01-01
Phase II study of afatinib for non-small cell lung cancer acquired resistance to osimertinib (North Japan Lung Cancer Study Group 1801)
CTID: UMIN000030399
Phase: Phase II    Status: Recruiting
Date: 2017-12-15
Afatinib alone or with bevacizumab as first-line therapy in patients with advanced non-squamous non-small-cell lung cancer harbouring active EGFR mutations : an open-label, randomized, multicenter, phase II study
CTID: UMIN000027432
Phase: Phase II    Status: Complete: follow-up complete
Date: 2017-06-18
A prospective, phase II trial of low-dose afatinib monotherapy for patients with EGFR, mutation-positive, non-small cell lung cancer(TORG1632).
CTID: UMIN000027338
Phase:    Status: Complete: follow-up complete
Date: 2017-05-15
A biomarker analysis of Afatinib treatment in patients with relapse of EGFR-T790M mutation-positive advanced lung adenocarcinoma after 3rd generation EGFR-TKI treatment.
CTID: UMIN000025126
Phase:    Status: Recruiting
Date: 2016-12-03
Resistant mechanisms to afatinib in non-small cell lung cancer with EGFR mutations
CTID: UMIN000024476
Phase:    Status: Recruiting
Date: 2016-10-19
Phase II study of low-dose afatinib for elderly patients with non-small cell lung cancer harboring EGFR mutation (based on TDM)
CTID: UMIN000022252
Phase: Phase II    Status: Recruiting
Date: 2016-05-10
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Biological Data
  • Afatinib (BIBW2992)

  • Afatinib (BIBW2992)
  • Afatinib (BIBW2992)

    Afatinib covalently binds to cysteine number 797 of the epidermal growth factor receptor (EGFR) via a Michael addition (IC50 = 0.5 nM).Schubert-Zsilavecz, M, Wurglics, M,Neue Arzneimittel Frühjahr 2013.(in German)

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